title: Pharmacokinetic interaction of fimasartan, a new angiotensin II receptor antagonist, with amlodipine in healthy volunteers.
abstract: OBJECTIVE
  Fimasartan (BR-A-657) is a new angiotensin II receptor antagonist used as antihypertensive agent. The objective of this study was to investigate the effect of the coadministration of fimasartan and amlodipine on the steady-state pharmacokinetics of each drug.
  
  
  METHODS
  This study comprised 2 separate parts, A and B; each was a multiple-dose, open-label, 2-period crossover study in healthy male volunteers. In part A, 20 subjects were administered 120 mg of fimasartan alone in period I and fimasartan with 10 mg of amlodipine in period II. In part B, 14 subjects were administered amlodipine alone, followed by coadministration with fimasartan. Blood samples for pharmacokinetics were collected up to 24 hours after the last dosing. The pharmacokinetics of the coadministration of fimasartan and amlodipine were compared with that of each drug alone.
  
  
  RESULTS
  The geometric mean ratio and 90% confidence intervals for C(max,ss) and area under the plasma concentration-time curve (AUC)(τ,ss) of fimasartan (with/without amlodipine) were 1.096 (0.746-1.610) and 1.163 (1.001-1.351), respectively. The geometric mean ratios (90% confidence interval) for C(max,ss) and AUC(τ,ss) of amlodipine (with/without fimasartan) after coadministration with fimasartan were 1.037 (0.969-1.110) and 0.975 (0.920-1.033), respectively.
  
  
  CONCLUSIONS
  Coadministration of fimasartan and amlodipine did not result in clinically relevant changes in the systemic exposure of fimasartan or amlodipine.
authors.affiliation: Department of Pharmacology and Clinical Pharmacology, Seoul National University College of Medicine and Hospital, Jongno-gu, Seoul, Republic of Korea.
authors.forename: SoJeong
authors.initials: S
authors.lastname: Yi
authors.forename: Tae-Eun
authors.initials: TE
authors.lastname: Kim
authors.forename: Seo Hyun
authors.initials: SH
authors.lastname: Yoon
authors.forename: Joo-Youn
authors.initials: JY
authors.lastname: Cho
authors.forename: Sang-Goo
authors.initials: SG
authors.lastname: Shin
authors.forename: In-Jin
authors.initials: IJ
authors.lastname: Jang
authors.forename: Kyung-Sang
authors.initials: KS
authors.lastname: Yu
mesh_terms: D000328:Adult; D000450:Aldosterone / Q000097:blood; D017311:Amlodipine / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D047228:Angiotensin II Type 1 Receptor Blockers / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D000959:Antihypertensive Agents / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D001713:Biphenyl Compounds / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D001794:Blood Pressure / Q000187:drug effects; D002121:Calcium Channel Blockers / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D018592:Cross-Over Studies; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions; D006801:Humans; D008297:Male; D008657:Metabolic Clearance Rate; D011743:Pyrimidines / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D012083:Renin / Q000097:blood; D013777:Tetrazoles / Q000008:administration & dosage / Q000009:adverse effects / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D047228:Angiotensin II Type 1 Receptor Blockers; D000959:Antihypertensive Agents; D001713:Biphenyl Compounds; D002121:Calcium Channel Blockers; D011743:Pyrimidines; D013777:Tetrazoles; D017311:Amlodipine; D000450:Aldosterone; D012083:Renin; C558933:fimasartan